Table 3.
Comparative Binding Affinity Data for Compound 13 and Agents currently in use at Human Receptors and Rat Transporters.
| a Receptor | Binding (Ki±SEM) Data of Compd 13 and standard agents at Selected Receptors (nM)b | ||||||
|---|---|---|---|---|---|---|---|
| Comp 13 | bClozapine | bRisperidone | bZiprasidone | bOlanzapine | bQuetiapine | bHaldol | |
| DA D1 | 162.7±33.1 | 290 | 580 | 130 | 52 | 1300 | 120 |
| DA D2 | 43.3±13.3 | 130 | 2.2 | 3.1 | 20 | 180 | 1.4 |
| DAD3 | 158.8±35.1 | 240 | 9.6 | 7.2 | 45 | 320 | 2.5 |
| DAD4 | 6.6±0.6 | 54 | 8.5 | 32 | 50 | 2200 | 3.3 |
| 5HT1A | 117.4±32.6 | 140 | 210 | 2.5 | 2100 | 230 | 3600 |
| 5HT2A | 23.6±2.7 | 8.9 | 0.29 | 0.39 | 3.3 | 220 | 120 |
| 5HT2B | 495.2±94.0 | NR | NR | NR | NR | NR | NR |
| 5HT2C | 1425.0±207 | 17 | 10 | 0.72 | 10 | 1400 | 4700 |
| 5HT6 | 295.9±48.6 | 11 | 2000 | 76 | 10 | 1400 | 6000 |
| Hist H1 | 188.6±16.0 | 1.8 | 19 | 47 | 2.8 | 8.7 | 440 |
| M1 | 871.6±75.6 | 1.8 | 2800 | 5100 | 4.7 | 100 | 1600 |
| DAT | 1150±133 | NR | NR | NR | NR | NR | NR |
| NET | 850.7±175.0 | 390 | 28000 | 48 | 2000 | 680 | 5500 |
| SERT | 56.6±6.0 | 3900 | 1400 | 53 | >15,000 | >18,000 | 1800 |
a
Human cloned receptors were used in all cases except for the NT transporters which are from rats.
b
Data for standard drugs were obtained from Schmidt et al., reference 12b.
NR = Not Reported.